申请人:WORLD HEALTH ORGANISATION
公开号:EP0129947A2
公开(公告)日:1985-01-02
A small group of esters of levo-norgestrel have been found to be unexpectedly effective as long term contraceptive agents. The esters are:
levo-norgestrel butanoate,
levo-norgestrel cyclopropylcarboxylate
levo-norgestrel cyclobutylcarboxylate
levo-norgestrel cyclopentylcarboxylate 3-oxime, or
levo-norgestrel cyclohexylcarboxylate 3-oxime
The esters may be formulated in a pharmaceutically acceptable aqueous medium, preferably in the form of a microcrystalline suspension of particle size in the range 3 to 10µ expressed as the 50% cumulative oversize in the Coulter distribution curve. A suitable human dosage 15 contains from 1 to 50 mgms of the ester.
研究发现,一小部分左炔诺孕酮酯类作为长期避孕药物具有意想不到的效果。这些酯类是
左炔诺孕酮丁酸酯、
左炔诺孕酮环丙基羧酸酯
左炔诺孕酮环丁基羧酸酯
左旋炔诺孕酮环戊基羧酸酯 3-肟,或
左旋炔诺孕酮环己基羧酸酯 3-肟
这些酯类可配制在药学上可接受的水介质中,最好是微晶悬浮液形式,粒度范围在 3 至 10µ 之间,用库尔特分布曲线中 50%的累积过大粒度表示。合适的人用剂量 15 含有 1 至 50 毫克酯。